Pharmacology Flashcards

(83 cards)

1
Q

sympathetic nervous system acts on __ receptors mediated by __ causing ___

A

B1 adrenoceptors
adrenaline and noradrenaline
increase in heart rate and contractility

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2
Q

sympathetic nerves innervate nodal and myocardial cells true/false

A

true

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3
Q

how do beta-adrenoceptors increase heart rate and contractility

A

activate G protein coupled receptors - activates adenylyl cyclase - increases cAMP - increases number of L-type channels - triggers release of calcium from SR

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4
Q

increase in heart rate is known as

A

positive chronotropic effect

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5
Q

increase in heart contractility is known as

A

positive inotropic effect

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6
Q

parasympathetic nervous system acts on __ mediated by __ causing ___

A

M2 muscarinic cholinoceptors
mediated by ACh
decrease in heart rate

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7
Q

parasympathetic nerves innervate nodal and myocardial cells true/false

A

false only on nodal cells - therefore only has effect on heart rate but not contractility

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8
Q

how does parasympathetic nerves decrease heart rate in nodal cells

A

when M2 binds to ACh making G protein - cAMP is reduced and potassium channels open decreasing contraction slope

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9
Q

what are the stages occurring for cardiac muscle contraction to occur

A

Ca L-type channels open during phase 2 - influx of Ca - triggers release of Ca from SR (CICR) - Ca binds to troponin C moving tropomyosin causing contraction

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10
Q

describe calcium induced calcium release

A

increasing the intracellular concentration of calcium causes further increase in its concentration from the sarcoplasmic reticulum

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11
Q

how does relaxation of cardiac muscle occur

A

repolarisation in phase 3 and 4 closes L-type channels. Ca influx stops and Ca dissociates from troponin C causing relaxation of muscle

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12
Q

what is the purpose of vagal manoeuvres

A

suppress conduction through the AVN - therefore decreasing heart rate

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13
Q

what are vagal manoeuvres used for

A

SVTs such as atrial fibrillation and atrial flutter

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14
Q

what is the funny current mediated by

A

HCN channels

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15
Q

which drug selectively blocks the HCN channel

A

ivabradine - decreasing slope on pacemaker potential

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16
Q

which conditions is ivabradine used for

A

angina - lowers oxygen requirements

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17
Q

which two areas can drugs act on to alter heart rate and contractility

A

beta-adrenoceptors

muscarinic receptors

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18
Q

what is the effect of B1 adrenoceptor agonists

A

activated adenylyl cyclase increasing cAMP which increases heart rate

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19
Q

name two examples of B-adrenoceptor agonists and their uses

A

dobutamine - IV for heart failure

adrenaline - cardiac arrest and anaphylaxis

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20
Q

what is the effect of beta-blockers

A

either selectively or non-selectively block beta-adrenoceptor slowing conduction through AVN reducing heart rate/oxygen requirement

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21
Q

name a non-selective beta-blocker and what does it act on

A

propanolol acting on B1 and B2 adrenoceptors

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22
Q

name some selective beta-blockers

A

atenolol, bisoprolol, metoprolol

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23
Q

what are the clinical uses of beta-blockers

A

angina
arrhythmias - esp AF
heart failure - start low and go slow as reduces sympathetic drive
(hypertension if extreme)

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24
Q

what are the side effects of beta-blockers

A
bradycardia 
can trigger bronchospasm esp in asthmatics 
fatigue
hypoglycaemia 
can aggravate heart failure 
cold extremities
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25
what is the effect of muscarinic ACh receptor antagonists
block parasympathetic action therefore increase heart rate
26
name two drugs that are muscarinic receptor antagonists
atropine | digoxin
27
what is the clinical use of atropine
used for extreme bradycardia following an MI
28
what is the clinical use of digoxin
treatment of heart failure as increases contractility
29
what are the side effects of digoxin
can cause heart block arrhythmias GI disturbances disturbance to colour vision
30
what are the classifications of drugs that have direct effect on vasculature and BP
organic nitrates calcium channel blockers ACEi and ARBs
31
how does smooth muscle contraction occur in vasculature
Ca through L-type channels activates MLCK causing contraction
32
how does relaxation occur in smooth muscle vasculature
myosin light chain phosphatase activated by protein kinase G causes relaxation of smooth muscle
33
what is the action of organic nitrates
organic nitrates metabolised into nitric oxide causing venorelaxation and arteriolar dilatation causing increased coronary blood flow
34
name a short acting organic nitrate and its use
GTN (glycerintrinitrate) administered sublingually | used for symptomatic relief of angina and acute MI
35
name a long acting organic nitrate and its use
isosorbide mononitrate administered orally | used for prophylaxis of angina
36
how can organic nitrates improve symptoms of angina
reduces myocardial oxygen requirement decreasing preload and afterload
37
what are some of the side effects of organic nitrates
over dilatation of blood vessels causing hypotension, headaches, dizziness and nausea
38
what is the effect of repeated administration of organic nitrates
can cause diminished effect - therefore nitrate free period overnight is recommended
39
which calcium channel blocker has an effect on cardiac L-type channels
verapamil
40
which calcium channel blocker has an effect on smooth muscle L-type channels
amlodipine
41
what is the overall effect of blocking Ca channels
reduction in intracellular Ca causing arteriolar dilatation
42
what are Ca channel blockers used for
hypertension angina arrhythmias
43
what are the side effects of calcium channel blockers
excessive vasodilation causing hypotension, dizziness and ANKLE OEDEMA
44
what is haemostasis
the stopping of blood flow through a damaged vessel
45
what is thrombosis
pathological haemostasis - formation of blood clot
46
thrombin from coagulation cascade is activated from ___ by ___ enzyme
prothrombin | prothrombinase
47
describe arterial thrombus
white thrombus mainly containing platelets
48
where is an arterial thrombus most likely to detach and travel to
heart arteries brain - stroke
49
describe venous thrombus
red thrombus mainly containing fibrin
50
where is a venous thrombus most likely to detach and travel to
lung from lower limbs
51
arterial thrombus is treated with
antiplatelets
52
venOus thrombus is treated with
anticOagulants
53
what is the mechanism of anticoagulants
block different points of the coagulation cascade typically prothrombinase, thrombin and factor Xa
54
name the clinical uses of anticoagulants
DVTs and PE atrial fibrillation prophylaxis post-op thrombosis
55
name some anticoagulants
warfarin rivaroxaban epixaban heparin
56
what type of drug is warfarin classed as
vitamin K antagonist
57
what is one of the major side effects of taking anticoagulants
increased risk of haemorrhage
58
what factors can lessen the effects of warfarin
anything increased risk of thrombosis: - pregnancy - hypothyroidism - vitamin K consumption (green salad vegetables)
59
which factors of the coagulations cascade does warfarin interact with
factor II, VII, IX and X
60
heparin and LMWHs are which type of anticoagulants
antithrombins
61
what is the mechanism of heparin
binds to antithrombin III increasing affinity for clotting factors
62
when is the only time heparin is preferred over LMWHs
when the patient has renal failure
63
name some examples of antiplatelets
aspirin clopidogrel ticagrelor
64
what are some of the side effects of antiplatelets
haemorrhage | aspirin also causes GI upset
65
when are fibrinolytic drugs used
as thrombolysis to reopen occluded arteries in acute stroke or MI
66
name an example of fibrinolytic drug
streptokinase
67
what causes renin to be released from the kidneys
drop in blood pressure - body thinks there is not enough fluid and so will retain it
68
what is ACE and its function
enzyme converting angiotensin I to angiotensin II | acts as a vasoconstrictor and inactivates bradykinin
69
what is bradykinin
vasodilator inactivated by ACE
70
what is the effect of an ACE inhibitor
blocking the conversion of angiotensin causes arteriolar dilatation and venous dilatation - overall reduces blood pressure and cardiac load
71
what is an ARB
angiotensin receptor blocker - very similar effect however doesn't activate bradykinin
72
what are the clinical uses of ACEis and ARBs
hypertension | heart failure following MI
73
what is a common side effect of an ACEi but not an ARB and why
dry cough due to the activation of bradykinin
74
are ACEis and ARBs safe in pregnancy
no as the have foetal toxicity
75
name two examples of alpha blockers
prazosin and doxazosin
76
what is the effect of alpha blockers
through blocking A1 channel throughout the rest of the body - sympathetic vasoconstriction is prevented - prevents blood pressure from getting too high
77
what is the indication for alpha blockers
severe hypertension | or patient with benign prostatic hyperplasia and hypertension
78
what is an adverse effect of alpha blockers
postural hypotension
79
what is the purpose of diuretics
acts on kidneys to increase Na, Cl and water excretion - indirectly relaxing vasculature
80
what are the two types of diuretics
thiazide diuretics | loop diuretics
81
give an example of a thiazide diuretic and its main uses
bendroflumethiazide | used mainly for hypertension as not as effective for removing fluid
82
give an example of a loop diuretic and its main uses
furosemide | has strong diuresis and used for acute pulmonary oedema and chronic heart failure
83
what are the main side effects of diuretics
can cause severe hypokalaemia and require K supplements or can lead to gout also thirst and dizziness